Do N-arachidonyl-glycine (NA-glycine) and 2-arachidonoyl glycerol (2-AG) share mode of action and the binding site on the β2 subunit of GABAA receptors?

Roland Baur; Jürg Gertsch; Erwin Sigel

doi:10.7717/peerj.149

Do N-arachidonyl-glycine (NA-glycine) and 2-arachidonoyl glycerol (2-AG) share mode of action and the binding site on the β2 subunit of GABAA receptors?

PeerJ. 2013 Sep 10:1:e149. doi: 10.7717/peerj.149. eCollection 2013.

Authors

Roland Baur¹, Jürg Gertsch, Erwin Sigel

Affiliation

¹ Institute of Biochemistry and Molecular Medicine, University of Bern , Bern , Switzerland.

Abstract

NA-glycine is an endogenous lipid molecule with analgesic properties, which is structurally similar to the endocannabinoids 2-AG and anandamide but does not interact with cannabinoid receptors. NA-glycine has been suggested to act at the G-protein coupled receptors GPR18 and GPR92. Recently, we have described that NA-glycine can also modulate recombinant α1β2γ2 GABAA receptors. Here we characterize in more detail this modulation and investigate the relationship of its binding site with that of the endocannabinoid 2-AG.

Keywords: 2-AG; Endocannabinoids; GABA; GABAA receptors; NA-glycine.

Grants and funding

This work was supported by the Swiss National Science Foundation grants 31003A_132806/1 (ES) and 31003A_120672 (JG). The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.